GNE-064（化合物5）是一款具有口服活性、高可溶性的选择性抑制剂，可靶向SMARCA4、SMARCA2及PBRM1bromodomains5，同时对SMARCA4（IC500.035μM）、SMARCA2（EC500.10μM）有明确抑制活性，对上述三个靶点及PBRM1bromodomains2的Kd值分别为0.01、0.016、0.018、0.049μM，还可作为活性分子探针用于活性分子合成研究。

[1] Taylor AM, Bailey C, Belmont LD, Campbell R, Cantone N, Côté A, Crawford TD, Cummings R, DeMent K, Duplessis M, Flynn M, Good AC, Huang HR, Joshi S, Leblanc Y, Murray J, Nasveschuk CG, Neiss A, Poy F, Romero FA, Sandy P, Tang Y, Tsui V, Zawadzke L, Sims RJ 3rd, Audia JE, Bellon SF, Magnuson SR, Albrecht BK, Cochran AG. GNE-064: A Potent, Selective, and Orally Bioavailable Chemical Probe for the Bromodomains of SMARCA2 and SMARCA4 and the Fifth Bromodomain of PBRM1. J Med Chem. 2022 Aug 25;65(16):11177-11186. doi: 10.1021/acs.jmedchem.2c00662. Epub 2022 Aug 5. PMID: 35930799.